Regioselective Synthesis Of 2,4-Diaryl-6-Trifluoromethylated Pyridines Through Copper-Catalyzed Cyclization Of Cf3-Ynones And Vinyl Azides

A novel copper-catalyzed cyclization of readily available vinyl azides with CF3-ynones is steadily achieved under mild conditions to furnish the versatile 2,4-diaryl-6-trifluoromethylated pyridine products, which are of great interest in medicinal chemistry. The generation of the vinyl iminophosphorane intermediates from vinyl azides through the Staudinger-Meyer reaction ensures the subsequent 1,4-addition process with CF3-ynones in this transformation.